| Autor: |
Gouault N; Faculté de Pharmacie, 35043 Rennes-cédex, France., Pinel B, Cupif JF, Depince A, Martin-Chouly CA, Belleguic C, David M |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2004 Dec; Vol. 19 (6), pp. 475-80. |
| DOI: |
10.1080/14756360412331280536 |
| Abstrakt: |
A solid-phase route for the preparation of 4a,5,8,8a-tetrahydrophthalazinon-1-ones employing the Diels-Alder reaction has been developed. Some of the new compounds have been tested for inhibition of LPS-stimulated TNF-alpha production in human whole blood from patients with chronic obstructive pulmonary disease (COPD). This evaluation revealed two compounds 17 and 18 of interest, incorporating an arylpiperazine moiety, which were found to inhibit LPS-induced TNF-alpha release like the well known anti-inflammatory PDE4 inhibitors, rolipram and roflumilast. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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